Department of Internal Medicine, Taipei Medical University Hospital, Taipei, Taiwan, ROC.
Pharmacology. 2010;85(3):131-5. doi: 10.1159/000280583. Epub 2010 Feb 9.
To determine the effect of an oral dose of sitagliptin on the secretion of ghrelin and gastrin hormones.
Ten healthy volunteers were recruited in this study. A baseline blood sample was drawn before oral dosing with a 100-mg tablet of sitagliptin. Two blood samples were obtained 0.5 and 1 h after dosing. Three additional postprandial blood samples were drawn at 0.5, 1, and 2 h. Radioimmunoassay was used for determining hormonal levels. A Student's t test, Pearson correlation analysis, and multivariate approach to repeated-measures analysis of variance were used for statistics.
After sitagliptin dosing, but before the meal, there was no significant change in circulating ghrelin, gastrin, insulin, and glucose levels. Only after meal loading was there a progressive and persistent decline in ghrelin levels until the end of the study, while a rapid and temporary rise in gastrin, insulin, and glucose levels at 0.5 h was observed. The levels of gastrin, insulin, and glucose then declined progressively.
Preprandial oral dose of sitagliptin does not affect circulating ghrelin, gastrin, insulin, and glucose concentrations in normal subjects. Decreased ghrelin and increased gastrin and insulin levels occurred only after meal loading. These results support the theory that sitagliptin might not cause appetite-enhanced body weight gain and insulin-induced hypoglycemia.
确定口服西他列汀对胃饥饿素和胃泌素激素分泌的影响。
本研究招募了 10 名健康志愿者。在口服 100mg 西他列汀片之前，抽取基线血样。给药后 0.5 和 1 小时采集 2 份血样。给药后 0.5、1 和 2 小时还采集了 3 份餐后血样。采用放射免疫法测定激素水平。采用学生 t 检验、皮尔逊相关分析和重复测量方差的多变量方法进行统计学分析。
西他列汀给药后，但在进餐前，循环中胃饥饿素、胃泌素、胰岛素和血糖水平没有显著变化。只有在进食负荷后，胃饥饿素水平才会逐渐持续下降，直至研究结束，而胃泌素、胰岛素和血糖水平在 0.5 小时会迅速暂时升高。然后，胃泌素、胰岛素和血糖水平逐渐下降。
正常受试者餐前口服西他列汀不会影响循环中胃饥饿素、胃泌素、胰岛素和血糖浓度。只有在进食负荷后才会出现胃饥饿素降低和胃泌素和胰岛素水平升高。这些结果支持西他列汀可能不会引起食欲增强体重增加和胰岛素引起的低血糖的理论。
